FOOD RESEARCH INTERNATIONAL
·
2025
·
IF 8
Jin Liang,Yanzhi Liu,Fengyi Liu,Xiaoying Zhang,Yue Su,Jun Wang,Fang Duan,Gang Wu,Kai Qiu
Microbial contamination and oxygen ingress are primary drivers of food spoilage, but advanced materials that simultaneously offer high oxygen barrier and effective antibacterial functions remain scarce. To address this dual challenge, we engineered a polyvinyl alcohol-based composite coating, incorporating the natural aggregation-induced emission photosensitizer berberine (BBR) and non-toxic layered double hydroxide nanosheets (LDH NS), on a polyethylene terephthalate substrate. The developed composite film demonstrated a low oxygen transmission rate of 0.06 cm 3 m −2 day −1 atm −1 . Furthermore, it achieved 100 % inhibition rate against both Staphylococcus aureus and Escherichia coli upon light irradiation. Crucially, we propose and elucidate a novel antimicrobial enhancement mechanism mediated by the orderly-arranged LDH NS for BBR. This mechanism involves (i) promoting BBR molecular aggregation to enhance reactive oxygen species (ROS) generation, and (ii) improving bacterial capture capacity via electrostatic interactions. These effects collectively establish a synergistic “capture–ROS enrichment–bacterial killing” pathway on the film surface. In a practical application, the composite film effectively suppressed microbial growth on packaged bread, extending its shelf life by more than 4-fold compared to conventional packaging. This work not only presents a promising multifunctional material for food preservation but also provides fundamental insights into the design of nanomaterial-enhanced, natural photosensitizer-based systems for advanced active packaging.
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CARBOHYDRATE POLYMERS
·
2025
·
IF 12.5
Min Qiu,Jiaxin Li,Huijuan Xie,Jiamin Feng,Qi Huang,Yin Tian,Haozhou Huang,Li Han,Dingkun Zhang
Bitterness masking is a crucial technical hurdle in the development and application of oral liquid medicines. Small-molecule excipients, such as cyclodextrin, often provide insufficient bitterness masking, thus prompting the exploration of large-molecule excipients, especially polysaccharides. In this study, the bitterness-masking effects of 10 polysaccharides were assessed using berberine as a model. Only iota-carrageenan significantly reduced the bitterness of berberine, decreasing it from strong to slight. A comparative study of the bitterness-masking mechanisms of three polysaccharides revealed that carrageenan polymer chains formed an interwoven network, decreasing the release of berberine by 40 %. Moreover, -OSO₃ − groups on the polymer chains exhibited strong electrostatic interactions with the N + in berberine, significantly reducing the electron cloud density of N + . This combined effect traps berberine within the “net-hook” structure of the iota-carrageenan, markedly weakening the activation of bitter receptors by the berberine. Ultrasonic treatment-induced disruption of the iota-carrageenan network structure yielded a 29 % reduction in bitterness-masking efficacy, while carrageenan with a lower -OSO₃ − content achieved a 40 % reduction in efficacy. In conclusion, the “net-hook” structure of natural polysaccharides is a necessary condition for them to exert a bitterness-masking effect. This finding provides a scientific basis for expanding the applications of natural polysaccharides in taste-masking.
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BioNanoScience
·
2026
·Vol. 16
·期 5
·320
·
IF 4
Ma Yingying,Xue Linying,Wang Yancai
Alzheimer’s disease (AD), a progressive neurodegenerative disorder, is the leading clinical cause of dementia. Magnolol has promising therapeutic potential for AD. However, its poor aqueous solubility and the challenge of achieving brain-targeted delivery have severely hindered its clinical usage. This study designed a thermosensitive in situ hydrogel nasal spray for co-delivery of magnolol nanosuspensions and berberine, targeting AD treatment via nose-to-brain delivery. The magnolol nanosuspensions were prepared via a wet-milling approach to improve the drug’s solubility. A thermosensitive hydrogel based on poly(N-isopropylacrylamide) (PNIPAM) was synthesized and formulated as an in situ nasal spray to enable brain-targeted co-delivery of the two drugs. In vitro PC12 cells AD models and in vivo mice was used to evaluation the thermosensitive multifunctional in-situ hybrid gel effectiveness and distribution. Morphological characterization confirmed successful preparation of magnolol nanosuspensions with a mean particle size of 220 ± 10 nm, which exhibited a high dissolution rate of 82.36 ± 1.62% within 300 min. The nanosuspensions were embedded in the hydrogel, which has a lower critical solution temperature (LCST) of approximately 32 °C - allowing rapid phase transition in the nasal cavity (local temperature ~ 35 °C). On PC12 cells and mice AD models, the thermosensitive hydrogel co-delivery system increased cell survival by 27.13% and significantly enhanced drug accumulation in the brain. This multifunctional drug delivery system provides an efficient strategy for the brain-targeted delivery of magnolol nanosuspensions and berberine, offering a promising approach for AD treatment.
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Frontiers in Neuroscience
·
2025
·
IF 3.2
Wei Liu,Ruheng Wei,Jingya Xu,Zhilong Liu,Yulai Li
Objective: Post-stroke depression (PSD), a common neuropsychiatric complication, significantly hinders stroke recovery and quality of life. Given the established role of inflammation in the pathogenesis of PSD, this study aimed to identify key inflammation-related genes and pathways using bioinformatics and machine learning and further evaluate the protective effects of traditional Chinese medicine (TCM) monomer compounds.Methods: PSD-related datasets (GSE16561, GSE98793) were obtained from the Gene Expression Omnibus (GEO). Differentially expressed genes (DEGs) were identified using the limma package, followed by functional enrichment analysis with Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG). Three machine learning algorithms—random forest, support vector machine-recursive feature elimination (SVM-RFE), and least absolute shrinkage and selection operator (LASSO)—were applied to screen inflammation-related hub genes. Immune cell infiltration was analyzed using single-sample gene set enrichment analysis (ssGSEA). Candidate TCM compounds were explored via the Coremine Medical database. A PSD rat model was established to validate hub gene expression and to assess the efficacy of berberine (BBR).Results: Analysis identified 35 inflammation-related DEGs (IDEGs) significantly enriched in immunological processes, including malaria pathogenesis, NETosis, innate immune deficiencies, Rap1 signaling, and IL-17 cascades. The integration of machine learning pinpointed TLR2 and CYP1B1 as core hub genes, demonstrating robust diagnostic performance in external validation. Molecular docking suggested a strong binding affinity between the TCM compound BBR and TLR2/CYP1B1 proteins. PSD rats exhibited prolonged immobility in forced swim/tail suspension tests and decreased sucrose preference versus controls, alongside neuronal damage, edema, and inflammatory infiltration (HE staining). BBR treatment reversed these behavioral deficits and pathological changes. Western blot analysis confirmed elevated TLR2 and CYP1B1 expression in PSD rats, significantly downregulated by BBR. Enzyme-linked immunosorbent assay (ELISA) showed increased serum IL-1β, IL-6, and TNF-α levels in PSD, which BBR effectively reduced.Conclusion: This study identifies TLR2 and CYP1B1 as core inflammation-related genes in PSD. BBR demonstrates therapeutic efficacy as an active monomer compound against PSD, likely mediated through downregulating TLR2 and CYP1B1 expression, consequently diminishing the concentrations of pro-inflammatory mediators (IL-1β, IL-6, TNF-α) that mediate cerebroprotective actions.
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MOLECULES
·
2024
·Vol. 29
·期 5
·1055
·
IF 4.2
Jing Xu,Xiu-Wei Yang
Berberine is a natural isoquinoline alkaloid with low toxicity, which exists in a wide variety of medicinal plants. Berberine has been demonstrated to exhibit potent prevention of indomethacin-induced gastric injury (GI) but the related mechanism remains unclear. In the present study, liquid chromatography-mass spectrometry (LC-MS)-based metabolomics was applied for the first time to investigate the alteration of serum metabolites in the protection of berberine against indomethacin-induced gastric injury in rats. Subsequently, bioinformatics was utilized to analyze the potential metabolic pathway of the anti-GI effect of berberine. The pharmacodynamic data indicated that berberine could ameliorate gastric pathological damage, inhibit the level of proinflammatory factors in serum, and increase the level of antioxidant factors in serum. The LC-MS-based metabolomics analysis conducted in this study demonstrated the presence of 57 differential metabolites in the serum of rats with induced GI caused by indomethacin, which was associated with 29 metabolic pathways. Moreover, the study revealed that berberine showed a significant impact on the differential metabolites, with 45 differential metabolites being reported between the model group and the group treated with berberine. The differential metabolites were associated with 24 metabolic pathways, and berberine administration regulated 14 of the 57 differential metabolites, affecting 14 of the 29 metabolic pathways. The primary metabolic pathways affected were glutathione metabolism and arachidonic acid metabolism. Based on the results, it can be concluded that berberine has a gastroprotective effect on the GI. This study is particularly significant since it is the first to elucidate the mechanism of berberine’s action on GI. The results suggest that berberine’s action may be related to energy metabolism, oxidative stress, and inflammation regulation. These findings may pave the way for the development of new therapeutic interventions for the prevention and management of NSAID-induced GI disorders.
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ChemistrySelect
·
2026
·Vol. 11
·期 14
·e05177
·
IF 2.3
Yin Wang,Kai Chen,Chao Lv,Dong Ju Zhou,Ya Wei Chen,Hui Yun Zhou,Hyun Jin Park
In this study, Ser-β-CD was synthesized, and BBH/Ser-β-CD IC was prepared by the freeze-drying method and characterized by FTIR, 1 H NMR, phase solubility, and SEM. Then, the BBH/Ser-β-CD IC@CS hydrogel was prepared by the BBH/Ser-β-CD IC and CS with GP as the crosslinking agent. The effect on hydrogel properties was investigated by altering (CS+BBH/Ser-β-CD IC) % (w/v), CS/(BBH/Ser-β-CD IC) (w/w), and (CS+BBH/Ser-β-CD IC)/GP (v/v). The FTIR results proved the interaction between hydrogel molecules. The SEM results confirmed the porous structure of the hydrogel. Meanwhile, hydrogels have been proven to have good swelling properties. The in vitro release results indicated that the hydrogel had a sustained-release effect, and the release mechanism of BBH from the hydrogel conformed to the first-order kinetic model. The DPPH scavenging capacity of hydrogels was comparable to that of Vc. The hemolysis test confirmed that the hydrogel had good biocompatibility. The antibacterial investigation proved that the hydrogel had an inhibitory effect on E. coli or S. aureus . Therefore, BBH/Ser-β-CD IC@CS hydrogel has broad prospects in the research and development of drug sustained-release and antibacterial materials. Graphical Ser-β-CD was synthesized, and BBH/Ser-β-CD IC was prepared by the freeze-drying method. BBH/Ser-β-CD IC@CS hydrogel was prepared using BBH/Ser-β-CD IC and CS with GP as a crosslinking agent. The BBH/Ser-β-CD IC@CS hydrogel had antioxidant properties, sustained-release performance, and antibacterial activity against E. coli and S. aureus .
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2026
·
IF 4.9
Dan Liu,Yaxian Yang,Jiacheng Meng,Honglei Guo,Xinchao Shi,Xin He,Xinghua Zhao
Berberine hydrochloride (BH) is a natural alkaloid compound known for its effectiveness in treating ulcerative colitis (UC). However, the clinical application of BH was limited due to the short half-life and rapid metabolism in body. Therefore, a sustained-release solid dispersion (SD) of BH was prepared using different proportions of ethyl cellulose as carrier. PXRD, DSC, and FT-IR analyses confirmed the transition of BH from a crystalline to amorphous state. This transformation significantly improved the drug release rate of BH and the pharmacokinetic characteristics in rats. The in vitro dissolution results showed that the cumulative dissolution rates of SD (1:4) were 29.47 % and 93.88 % at 10 min and 24 h respectively, and the in vivo study demonstrated that the t 1/2 (0−24) and the AUC 0−24 of SD (1:4) were 5.52 times and 6.30 times greater than those of BH, respectively, indicating SD (1:4) superior sustained-release effect compared to BH. In the acetic acid (AA)-induced UC rat model, SD treatment alleviates UC by increasing colon length, improving pathological damage, and reducing both the DAI score and levels of inflammatory factors. The 16S rRNA sequencing results indicated that SD treatment reshaped gut microbiota in rats with UC, particularly increasing the abundance of probiotic Romboutsia and decreasing the abundance of pathogenic bacteria Erysipelotrichaceae , Clostridia_UCG_014 and Dubosiella . In conclusion, we successfully prepared a sustained-release SD of BH and demonstrated that its therapeutic effect on UC is achieved by regulating intestinal microbiota.
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Dose-Response
·
2020
·
IF 2.438
Bing Han,Kai Wang,Yanbei Tu,Lihua Tan,Chengwei He
Berberine (BBR), a major active component of Rhizoma coptidis , is one of the most promising agents for breast cancer adjuvant therapy. It is well accepted that BBR could exhibit remarkable anticancer efficacy with few side effects, and when treated with chemotherapeutic agents in combination, BBR could enhance the chemosensitivity of cancer cells. Our previous study reported that low-dose BBR (LDB) induced hormetic effect and attenuated the anticancer activity of chemotherapeutic agents. However, the underlying mechanisms are still unclear. In this study, we confirmed that LDB could promote cancer cell proliferation and antagonize the anti-breast cancer activities of chemotherapeutic agents. And the mechanisms were proved to be induction of autophagy and antioxidation by LDB. Our results showed that LDB could mildly induce reactive oxygen species, raise the level of autophagy by promoting the phosphorylation of adenosine monophosphate-activated protein kinase, and promote antioxidant enzymes expression through activating nuclear factor erythroid 2-related factor 2 in breast cancer cells. These findings revealed a potential negative impact of BBR on its adjuvant anti-breast cancer therapy, providing guidance for a safe and effective use of naturally originated medicines in the clinic.
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ACS Applied Materials & Interfaces
·
2019
·
IF 8.456
Xuemei Huang,Penglong Wang,Tong Li,Xuehao Tian,Wenbo Guo,Bing Xu,Guangrui Huang,Desheng Cai,Fei Zhou,Hao Zhang,Haimin Lei
S. aureus is resistant to various first-line antibiotics, and seeking multifarious strategies aimed at effective control of antibiotic-resistant behavior is urgently needed. Here, we report a two-component directed self-assembly mode: the phytochemicals berberine and cinnamic acid can directly self-assemble into nanoparticles (NPs) displaying good bacteriostastic activity. Compared with several first-line antibiotics, the obtained nanostructures have a better inhibitory effect on multidrug-resistant S. aureus (MRSA) and stronger ability for biofilm removal. These qualities are attributed to the fact that organic assemblies can first spontaneously adhere to the surface of the bacteria, infiltrate into the cell, and then lead to converging attack against MRSA; thereafter, multipath bactericidal mechanisms of NPs on MRSA are found by both transcriptomic analysis and quantitative Polymerase Chain Reaction analysis. Moreover, when combined with spectral data and single crystal X-ray diffraction, the NPs’ self-assembly mechanism governed by hydrogen bonds and π–π stacking interactions is clearly elucidated. These non-covalent interactions induce the NPs’ formation of butterfly-like one-dimensional self-assembled units and finally layered three-dimensional spatial configuration. In addition, biocompatibility tests show that the NPs are nonhemolytic with little toxicity in vitro and in vivo. This directed self-assembly mode can offer a new perspective toward the design of biocompatible antimicrobial nanomedicines for clinical translation.
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Oxidative Medicine and Cellular Longevity
·
2018
·
IF 4.936
Hong-Xin Cui,Ya-Nan Hu,Jing-Wan Li,Ke Yuan
Both alterations to the intestinal microflora and chronic systemic inflammation predispose towards type 2 diabetes (T2D). Changes in the composition of the intestinal microflora are associated with glucose metabolism changes in rats with T2D. Here, we demonstrate that a berberine fumarate (BF) has a hypoglycemic effect by regulating the intestinal microflora and metabolism of diabetic rats. The T2D rats had disorders of glucose and lipid metabolism, an abnormal intestinal microflora, fewer butyrate-producing and probiotic-type bacteria, larger numbers of potentially pathogenic and sulfate-reducing bacteria, and tissue inflammation. Administration of berberine fumarate significantly ameliorated the metabolic disorder; increased the populations of Bacteroidetes, Clostridia, Lactobacillales, Prevotellaceae, and Alloprevotella; and reduced those of Bacteroidales, Lachnospiraceae, Rikenellaceae, and Desulfovibrio. In addition, it reduced inflammation, inhibiting the overexpression of TLR4 and p-JNK and increasing the expression of PI3K, GLUT2, and other proteins, which are closely related to oxidative stress, thereby promoting the metabolism of glucose.
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CHEMICAL ENGINEERING JOURNAL
·
2019
·
IF 8.355
Yizhen Zhang,Lifen Liu,Bart Van der Bruggen,Michael K.H. Leung,Fenglin Yang
Berberine is a widely used antibiotic in China, its photocatalytic degradation is not well understood nor its efficient treatment reported. In this study, it is most quickly and efficiently degraded (97.9% under UV and 98.9% under visible light) using a free-standing 3D composite photo-electrode, with well dispersed Ag nanoparticles (Ag NPs) over well-aligned ZnO nanorods arrays (ZnO NAs) on Ni foam (NiF), compared to ZnO NAs/NiF, ZnO powder and P25. The composite photo-electrode was prepared by first directly growing ZnO NAs on NiF hydrothermally, followed by photo-deposition of Ag NPs, without any inactive binders or non-conductive substrates. It was characterized using scanning electron microscope (SEM), X-ray photoelectron spectroscopy (XPS), X-ray Diffraction (XRD), ultraviolet–visible spectrophotometry (UV–Vis) and electrochemical analysis (I-t, EIS). The highest activity of Ag NPs/ZnO NAs/NiF in degrading the target pollutant, is due to the synergy of easy pollutants diffusion and fast reaction on active sites, from suppressed electron-hole recombination by Ag NPs/ZnO NAs heterojunctions, extended light absorption by surface plasmon resonance (SPR) of Ag NPs and accelerated electron transport on the conductive macro-porous NiF. The reactive oxidizing species ( OH, O 2 − , h ± ), degradation intermediates and possible degradation pathways of berberine over Ag NPs/ZnO NAs/NiF were examined respectively. This free-standing whole piece photo-electrode with UV–visible light response, is easy to recycle and assemble, that not only degrades pollutant, but also generates electricity as photo-anode in a photo-catalytic fuel cell reactor using carbon fiber cloth as cathode.
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Polymers
·
2018
·Vol. 10
·期 11
·1198
·
IF 2.935
Jingfu Jia,Kerong Zhang,Xue Zhou,Dan Zhou,Fahuan Ge
It is still controversial whether poor aqueous solubility is the most primary reason for the low oral bioavailability of insoluble drugs. Therefore, in this study, berberine-loaded solid polymeric particles (BPs) of varied dissolution profiles with β-cyclodextrin (β-CD) as carrier were fabricated using solution-enhanced dispersion by supercritical fluids (SEDS), and the relationship between dissolution and berberine (BBR) bioavailability was evaluated. Dissolution property was controlled via particle morphology manipulation, which was achieved by adjusting several key operating parameters during the SEDS process. Characterization on BP using infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction indicated that BBR was dispersed in amorphous form, while nuclear magnetic resonance spectroscopy showed that methoxy groups of BBR were included into the cavities of β-CD. In vivo pharmacokinetic studies showed that oral bioavailability increased by about 54% and 86% when the dissolution rate of BBR was increased by 51% and 83%, respectively. The entry speed of BBR into the bloodstream was also advanced with the degree of dissolution enhancement. It seemed that dissolution enhancement gave positive effect to the oral bioavailability of berberine, but this might not be the crucial point. Meanwhile, supercritical CO2technology is a promising method for pharmaceutical research due to its advantages in regulating drug-dosage properties.Keywords:berberine;polymeric particle;supercritical CO2;dissolution;bioavailability
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